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1. 发明授权

US5523303A Trisubstituted cycloalkane derivatives and process for the preparation thereof 失效
标题翻译：三取代环烷烃衍生物及其制备方法
公开(公告)号：US5523303A
公开(公告)日：1996-06-04
申请号：US226051
申请日：1994-04-11
申请人： Judit Bajnogel , Gabor Blasko , Zoltan Budai , Andras Egyed , Marton Fekete , Erika Karaffa , Tibor Mezei , Klara Reiter nee Esses , Gyula Simig , Katalin Szemeredi , Eniko Szirt nee Kiszelly
发明人： Judit Bajnogel , Gabor Blasko , Zoltan Budai , Andras Egyed , Marton Fekete , Erika Karaffa , Tibor Mezei , Klara Reiter nee Esses , Gyula Simig , Katalin Szemeredi , Eniko Szirt nee Kiszelly
IPC分类号： A61K31/15 , A61K31/357 , A61K31/36 , A61K31/395 , A61K31/40 , A61K31/445 , A61K31/495 , A61K31/535 , A61K31/5375 , A61K31/55 , A61P1/04 , C07C249/12 , C07C251/58 , C07D295/08 , C07D295/088 , C07D317/58
CPC分类号： C07D295/088 , C07C251/58 , C07C2101/08 , C07C2101/14 , C07C2101/18 , Y10S514/925 , Y10S514/926 , Y10S514/927 , Y10S514/928
摘要： The invention relates to novel, pharmaceutically active trisubstituted cycloalkane derivatives, a process for the preparation thereof and pharmaceutical compositions comprising the same. The invention also encompasses the use of the said cycloalkane derivatives for the treatment of diseases and for the preparation of pharmaceutical compositions suitable for the treatment of diseases.The compounds according to the invention are characterized by the general formula (I), ##STR1## wherein R represents hydrogen, C.sub.1-4 alkyl or hydroxyl,R.sup.1 stands for C.sub.1-12 alkyl,R.sup.2 and R.sup.3 each represents hydrogen, C.sub.1-12 alkyl or C.sub.2-12 alkenyl, orR.sup.2 and R.sup.3 together with the adjacent nitrogen atom form a 4- to 7-membered ring optionally comprising an oxygen, sulfur or a further nitrogen atom, which latter may carry a phenyl, benzyl or C.sub.1-4 alkyl substituent,R.sup.4 and R.sup.5 each stands for hydrogen, halogen or C.sub.1-4 alkoxy, or together represent a 3,4-methylenedioxy group,n is an integer from 2 to 5,A represents a valency bond or a --CH.sub.2 -- group.The compounds exert a valuable antiulcer effect, so they can be used to advantage in the therapy.
摘要翻译：本发明涉及新颖的药学活性三取代环烷烃衍生物，其制备方法和包含其的药物组合物。本发明还包括所述环烷烃衍生物用于治疗疾病和制备适于治疗疾病的药物组合物的用途。根据本发明的化合物的特征在于通式（I），其中R表示氢，C 1-4烷基或羟基，R 1表示C 1-12烷基，R 2和R 3各自表示氢，C 1 -12烷基或C2-12烯基，或R2和R3与相邻的氮原子一起形成任选地包含氧，硫或另外的氮原子的4-至7-元环，后者可以携带苯基，苄基或C1 -4-烷基取代基，R4和R5各自代表氢，卤素或C1-4烷氧基，或一起代表3,4-亚甲二氧基，n是2至5的整数，A表示价键或-CH 2 - 组。这些化合物具有有价值的抗溃疡作用，因此可用于治疗。

2. 发明授权

US5597822A Pharmaceutical compositions for the prevention and/or treatment a gastrointestinal diseases 失效
标题翻译：用于预防和/或治疗胃肠道疾病的药物组合物
公开(公告)号：US5597822A
公开(公告)日：1997-01-28
申请号：US443487
申请日：1995-05-18
申请人： Eniko Szirt nee Kislelly , Zoltan Budai , Tibor Mezei , Gabor Blasko , Klara Kazo nee Daroczi , Andras Egyed , Gabor Gigler , Marton Fekete , Klara Reiter nee Esses , Gyula Simig , Katalin Szemeredi
发明人： Eniko Szirt nee Kislelly , Zoltan Budai , Tibor Mezei , Gabor Blasko , Klara Kazo nee Daroczi , Andras Egyed , Gabor Gigler , Marton Fekete , Klara Reiter nee Esses , Gyula Simig , Katalin Szemeredi
IPC分类号： A61K31/15 , A61K31/495 , A61K31/50 , A61K31/505
CPC分类号： A61K31/15 , A61K31/495
摘要： The invention refers to pharmaceutical compositions for the prevention and/or treatment of gastrointestinal diseases connected with infections caused by Helicobacter pylori and a method for the treatment of such diseases.The pharmaceutical composition of the invention comprises as active ingredient a cyclic ketone derivative of the formula I ##STR1## wherein and R.sup.1 mean independently hydrogen or halo;R.sup.0 stands for hydrogen or a C.sub.1-4 alkoxy group;R.sup.2 and R.sup.3 independently represent hydrogen; a straight or branched chain C.sub.1-8 alkyl optionally substituted by a dimethylamino group; a C.sub.2-6 alkenyl or a C.sub.3-7 cycloalkyl group; orR.sup.2 and R.sup.3 together with the adjacent nitrogen atom form a 6-membered heterocyclic group containing an additional nitrogen atom that may bear a phenyl group optionally substituted by a C.sub.1-4 alkoxy group;or its stereoisomer or optical isomer or a possible mixture thereof, or a pharmaceutically acceptable acid addition salt or quaternary ammonium salt thereof in admixture with carrier(s) commonly used in pharmaceutical compositions.
摘要翻译：本发明涉及用于预防和/或治疗与由幽门螺杆菌引起的感染有关的胃肠道疾病的药物组合物和治疗这些疾病的方法。本发明的药物组合物包含作为活性成分的式I（I）的环酮衍生物，其中R 1独立地表示氢或卤素; R0表示氢或C1-4烷氧基; R2和R3独立地表示氢; 任选被二甲基氨基取代的直链或支链C 1-8烷基; C 2-6烯基或C 3-7环烷基; 或者R 2和R 3与相邻的氮原子一起形成含有另外的氮原子的6元杂环基，其可以具有任选被C 1-4烷氧基取代的苯基; 或其立体异构体或光学异构体或其可能的混合物，或其药学上可接受的酸加成盐或季铵盐与药物组合物中通常使用的载体混合。

3. 发明授权

US5439940A Benz[e]indene derivatives 失效
标题翻译：苯并[e]茚衍生物
公开(公告)号：US5439940A
公开(公告)日：1995-08-08
申请号：US141954
申请日：1993-10-28
申请人： Klara Reiter nee Eszes , Zoltan Budai , Tibor Mezei , Gabor Blasko , Gyula Simig , Istvan Gyertyan , Luiza Petocz , Marton Fekete , Katalin Szemeredi , Istvan Gacsalyi , Gabor Gigler , Ludmilla Rohacas nee Zamkovaja , Maria Szecsey nee Hegedus , Eniko Szirt nee Kiszelly
发明人： Klara Reiter nee Eszes , Zoltan Budai , Tibor Mezei , Gabor Blasko , Gyula Simig , Istvan Gyertyan , Luiza Petocz , Marton Fekete , Katalin Szemeredi , Istvan Gacsalyi , Gabor Gigler , Ludmilla Rohacas nee Zamkovaja , Maria Szecsey nee Hegedus , Eniko Szirt nee Kiszelly
IPC分类号： A61K31/15 , A61K31/16 , A61K31/335 , A61K31/336 , A61K31/395 , A61K31/40 , A61K31/403 , A61K31/4035 , A61K31/44 , A61K31/4402 , A61K31/4427 , A61K31/495 , A61P25/04 , A61P25/20 , A61P29/00 , C07C13/547 , C07C249/04 , C07C251/58 , C07C269/02 , C07C271/60 , C07D209/48 , C07D213/74 , C07D239/24 , C07D239/34 , C07D241/04 , C07D295/08 , C07D295/088 , C07D303/12 , C07D401/02 , C07D401/04 , C07C251/54
CPC分类号： C07D209/48 , C07C251/58 , C07C271/60 , C07D213/74 , C07D239/34 , C07D295/088 , C07D303/12 , C07C2101/02 , C07C2101/14 , C07C2103/16
摘要： The invention relates to novel, pharmaceutically active benz[e]indene derivatives, a process for the preparation thereof, pharmaceutical compositions comprising the same, further to the use of the said benz[e]indene derivatives in the treatment of certain diseases and in the preparation of pharmaceutical compositions suitable for the treatment of said diseases.The new benz[e]indene derivatives according to the invention correspond to the general formula ##STR1## wherein A represents a group of the formula alk-NR.sup.1 R.sup.2, wherein alk represents a C.sub.2-7 alkylene group optionally carrying a hydroxy substituent,R.sup.1 and R.sup.2 are independently hydrogen, C.sub.1-7 alkyl, C.sub.2-7 alkenyl, C.sub.2-7 alkynyl, mono(C.sub.1-7)alkylamino(C.sub.1-7)alkyl, di(C.sub.1-7)alkylamino(C.sub.1-7)alkyl or C.sub.3-7 cycloalkyl; orR.sup.1 and R.sup.2 together with the nitrogen atom to which they are attached form a 4 to 7 membered ring, optionally comprising an oxygen atom or a further nitrogen atom, which latter may carry a phenyl, benzyl, pyridyl, pyrimidinyl or C.sub.1-3 alkyl substituent which substituents may, in turn, bear a hydroxy or methoxy group or a halogen atom or a halophenyl group; orR.sup.1 and R.sup.2 together with the nitrogen atom to which they are attached form a phthalimido group; orA represents pyrimidino, 2,3-epoxypropyl or a group of the formula --C(O)NHR.sup.3, whereinR.sup.3 stands for C.sub.1-7 alkyl, C.sub.2-7 alkenyl or C.sub.3-8 cycloalkyl; andR denotes hydrogen or C.sub.1-7 alkyl,stereoisomers and optically active isomers and the possible mixtures thereof, further acid addition salts and quaternary ammonium derivatives of these compounds.
摘要翻译：本发明涉及新的药学活性苯并[e]茚衍生物，其制备方法，包含其的药物组合物，进一步使用所述苯并[e]茚衍生物在某些疾病的治疗中以及在制备适于治疗所述疾病的药物组合物。根据本发明的新的苯并[e]茚衍生物对应于通式（I）其中A表示式alk-NR1R2的基团，其中alk表示任选携带羟基取代基的C 2-7亚烷基， R1和R2独立地是氢，C1-7烷基，C2-7烯基，C2-7炔基，单（C1-7）烷基氨基（C1-7）烷基，二（C1-7）烷基氨基（C1-7）烷基或 C3-7环烷基; 或R 1和R 2与它们所连接的氮原子一起形成4至7元环，任选地包含氧原子或另外的氮原子，后者可以携带苯基，苄基，吡啶基，嘧啶基或C 1-3烷基取代基，其取代基又可以具有羟基或甲氧基或卤素原子或卤代苯基; 或R 1和R 2与它们所连接的氮原子一起形成苯二甲酰亚氨基; 或A表示嘧啶基，2,3-环氧丙基或式-C（O）NHR 3的基团，其中R 3表示C 1-7烷基，C 2-7烯基或C 3-8环烷基; R表示氢或C 1-7烷基，立体异构体和旋光异构体及其可能的混合物，这些化合物的其它酸加成盐和季铵衍生物。

4. 发明授权

US5486528A Basic ethers and process for the preparation thereof 失效
标题翻译：碱性醚及其制备方法
公开(公告)号：US5486528A
公开(公告)日：1996-01-23
申请号：US226089
申请日：1994-04-11
申请人： Judit Bajnogel , Gabor Blasko , Zoltan Budai , Eva Schmidt , Andras Egyed , Marton Fekete , Istvan Gacsalyi , Istvan Gyertyan , Tibor Mezei , Kalara Reiter nee Esses , Gyula Simig , Katalin Szemeredi , Enik Szirt nee Kiszelly
发明人： Judit Bajnogel , Gabor Blasko , Zoltan Budai , Eva Schmidt , Andras Egyed , Marton Fekete , Istvan Gacsalyi , Istvan Gyertyan , Tibor Mezei , Kalara Reiter nee Esses , Gyula Simig , Katalin Szemeredi , Enik Szirt nee Kiszelly
IPC分类号： A61K31/135 , A61K31/15 , A61K31/357 , A61K31/36 , A61K31/395 , A61K31/40 , A61K31/44 , A61K31/4406 , A61K31/4418 , A61K31/445 , A61K31/495 , A61P1/04 , A61P25/20 , C07C251/32 , C07C251/58 , C07D207/08 , C07D213/30 , C07D295/00 , C07D295/08 , C07D295/088 , C07D317/58 , C07D405/12 , C07C251/48
CPC分类号： C07D207/08 , C07C251/58 , C07D295/088 , C07C2101/02 , C07C2101/14
摘要： Novel basic ether of general formula (I), ##STR1## wherein R.sup.1 and R.sup.2 are independently hydrogen, halogen or C.sub.1-4 alkoxy, or together they represent a 3,4-methylenedioxy group,R stands for C.sub.1-8 alkyl,R.sup.3 represents hydrogen, C.sub.1-4 alkyl or hydroxy,A is a valency bond or methylene group,R.sup.4 and R.sup.5 are independently hydrogen, C.sub.1-12 alkyl or C.sub.1-12 alkenyl, orR.sup.4 and R.sup.5 form together with the adjacent nitrogen atom 1-pyrrolidinyl, 1-piperidinyl, morpholino or 1-piperazinyl groups, stereo and optically active isomers and their possible mixtures, acid-addition salts and quaternary ammonium derivatives thereof. The basic ethers have antiulceric and anxiolytic activities.
摘要翻译：新型通式（I）的基本醚，其中R 1和R 2独立地为氢，卤素或C 1-4烷氧基，或一起它们代表3,4-亚甲二氧基，R代表C1-8烷基，R3代表氢，C1-4烷基或羟基，A是价键或亚甲基，R4和R5独立地是氢，C1-12烷基或C1-12烯基，或R4和R5与相邻的氮原子1一起形成吡咯烷基，1-哌啶基，吗啉代或1-哌嗪基，立体和旋光异构体及其可能的混合物，其酸加成盐和季铵衍生物。碱性醚具有抗溃疡和抗焦虑作用。

5. 发明授权

US5652270A Pharmaceutical compositions containing bicycloheptane ether amines and a process for the preparation thereof 失效
标题翻译：含有双环庚烷醚胺的药物组合物及其制备方法
公开(公告)号：US5652270A
公开(公告)日：1997-07-29
申请号：US664804
申请日：1996-06-17
申请人： Zoltan Budai , Istvan Gacsalyi , Gabor Szenasi , Tibor Mezei , Aniko Kovacs , Gabor Blasko , Katalin Szemeredi , Gyula Simig , Lujza Petocz , Klara Reiter nee Esses
发明人： Zoltan Budai , Istvan Gacsalyi , Gabor Szenasi , Tibor Mezei , Aniko Kovacs , Gabor Blasko , Katalin Szemeredi , Gyula Simig , Lujza Petocz , Klara Reiter nee Esses
IPC分类号： A61K31/135 , A61K31/54 , A61K31/445 , A61K31/495
CPC分类号： A61K31/135
摘要： The invention refers to a pharmaceutical composition, a process for the preparation thereof and a novel medical use of bicycloheptane derivatives. The pharmaceutical compositions of the invention comprise a bicycloheptane derivative of the formula I ##STR1## wherein said derivative is as defined in the specification herein. The pharmaceutical compositions of the invention are suitable for the treatment of diseases and disorders that are connected with the influence on the cholecystokinin system, especially for preventing the spastic contraction of the gallbladder.
摘要翻译：本发明涉及药物组合物，其制备方法和双环庚烷衍生物的新型医疗用途。本发明的药物组合物包含本说明书中所述的式I的双环庚烷衍生物。本发明的药物组合物适用于治疗与缩胆囊素系统的影响相关的疾病和病症，特别是用于防止胆囊的痉挛性收缩。

6. 发明授权

US5889018A Heterocyclic compounds, pharmaceutical compositions comprising them and process for the preparation thereof 失效
标题翻译：杂环化合物，包含它们的药物组合物及其制备方法
公开(公告)号：US5889018A
公开(公告)日：1999-03-30
申请号：US433120
申请日：1995-05-03
申请人： Gyula Balogh, deceased , Imre Doman , Gabor Blasko , Gyula Simig , Erzsebet Kovacs nee Kaszab , Istvan Gyertyan , Andras Egyed , Istvan Gacsalyi , Andras Bilkei-Gorzo , Katalin Pallagi , Katalin Szemeredi , Klara Kazo nee Daroczi
发明人： Gyula Balogh, deceased , Imre Doman , Gabor Blasko , Gyula Simig , Erzsebet Kovacs nee Kaszab , Istvan Gyertyan , Andras Egyed , Istvan Gacsalyi , Andras Bilkei-Gorzo , Katalin Pallagi , Katalin Szemeredi , Klara Kazo nee Daroczi
IPC分类号： C07D217/18 , A61K31/47 , A61K31/472 , A61P25/20 , C07D217/14 , C07D217/16 , C07D401/06 , C07D405/06 , C07D409/06 , C07D491/04 , C07D491/056 , A61K31/44
CPC分类号： C07D401/06 , C07D217/14 , C07D217/16 , C07D405/06 , C07D491/04
摘要： The invention relates to anxiolytic pharmaceutical compositions comprising as active ingredient 1-sytrylisoquinoline derivatives of general formula (I), whereinn is 1, 2, 3 or 4;R may be the same or different and represent(s) hydrogen, lower alkyl, lower alkoxy or hydroxy, or two substituents R attached to adjacent carbon atoms may form together an alkylenedioxy group;R.sup.1 represents hydrogen or lower alkyl, andAr stands for an optionally substituted aryl or heteroaryl,Some of the compounds of general formula (I) is known, but the majority thereof has not so far described in the literature.The invention also encompasses the preparation of the new compounds of general formula (I), which comprises reacting a compound of general formula (II) with an aldehyde or general formula (III) in the presence of a condensing agent or an acidic catalyst.
摘要翻译：本发明涉及抗焦虑药物组合物，其包含作为活性成分的通式（I）的1-对羟基异喹啉衍生物，其中n为1,2,3或4; R可以相同或不同，表示氢，低级烷基，低级烷氧基或羟基，或两个与相邻碳原子连接的取代基R可以一起形成亚烷基二氧基; R1表示氢或低级烷基，Ar表示任选取代的芳基或杂芳基。一些通式（I）的化合物是已知的，但其大部分尚未在文献中描述。本发明还包括通式（I）的新化合物的制备，其包括在缩合剂或酸性催化剂的存在下使通式（II）的化合物与醛或通式（III）反应。

7. 发明授权

US5716986A Oxaindene derivatives and process for the preparation thereof 失效
标题翻译：氧化烯衍生物及其制备方法
公开(公告)号：US5716986A
公开(公告)日：1998-02-10
申请号：US671515
申请日：1996-06-27
申请人： Csaba Szantay , Lajos Novak , Peter Kovacs , Klara Gado , Gabor Gigler , Julianna Takacs nee Bitai , Andras Egyed , Daniel Bozsing , Gyorgy Pirok , Katalin Szemeredi , Margit Csorgo , Sandor Drabant , Gabor Blasko , Gyula Simig , Gabor Kovacs
发明人： Csaba Szantay , Lajos Novak , Peter Kovacs , Klara Gado , Gabor Gigler , Julianna Takacs nee Bitai , Andras Egyed , Daniel Bozsing , Gyorgy Pirok , Katalin Szemeredi , Margit Csorgo , Sandor Drabant , Gabor Blasko , Gyula Simig , Gabor Kovacs
IPC分类号： C07D307/79 , A61K31/34 , A61K31/343 , A61K31/445 , A61K31/535 , A61P1/00 , A61P13/02 , A61P15/00 , A61P17/00 , A61P29/00 , A61P37/08 , C07D307/91 , C07D307/93
CPC分类号： C07D307/91 , C07D307/93
摘要： This invention relates to new oxaindene derivatives, a process for the preparation thereof and pharmaceutical compositions comprising the same. The compounds according to the invention are characterized by the general formula (1) ##STR1## wherein R.sup.1 represents lower C.sub.1-4 alkyl, lower C.sub.1-4 alkoxy or lower C.sub.3-6 cycloalkyl, R.sup.2 stands for hydrogen, lower C.sub.1-4 alkyl or lower C.sub.3-6 cycloalkyl, R.sup.3 stands for hydrogen, lower C.sub.1-4 alkyl, lower C.sub.1-4 alkoxy or benzyloxy, X denotes hydrogen, an aliphatic C.sub.1-4 -acyl or benzoyl or naphthoyl group, optionally substituted by 1 or more nitro or C.sub.1-4 -alkoxy group(s) or a group of the formula R.sup.5 R.sup.6 N--R.sup.7 --, wherein R.sup.7 represents lower C.sub.1-4 alkylene and R.sup.5 and R.sup.6 each represent lower C.sub.1-4 alkyl, or R.sup.5 and R.sup.6 together with the nitrogen atom to which they are attached form a piperidyl or morpholinyl group, A and B together form an ethylene or a vinylene group, and n is 1, 2 or 3, and have a strong 5-lipoxygenase (5-LO) enzyme inhibiting activity.
摘要翻译：本发明涉及新的氧杂茚衍生物，其制备方法和包含其的药物组合物。根据本发明的化合物的特征在于通式（1）其中R 1表示低级C 1-4烷基，低级C 1-4烷氧基或低级C 3-6环烷基，R 2表示氢，低级C 1〜 4烷基或低级C3-6环烷基，R3代表氢，低级C1-4烷基，低级C1-4烷氧基或苄氧基，X表示氢，脂族C1-4酰基或苯甲酰基或萘甲酰基，任选被1或更多的硝基或C 1-4 - 烷氧基或式R 5 R 6 N-R 7 - 的基团，其中R 7表示低级C 1-4亚烷基，R 5和R 6各自表示低级C 1-4烷基，或者R 5和R 6连同它们所连接的氮原子形成哌啶基或吗啉基，A和B一起形成乙烯或亚乙烯基，n为1,2或3，具有强的5-脂氧合酶（5-LO）酶抑制活性。

8. 发明授权

US5395934A 3(2H)-pyridazinone derivatives and process for the preparation thereof 失效
标题翻译： 3（2H） - 哒嗪酮衍生物及其制备方法
公开(公告)号：US5395934A
公开(公告)日：1995-03-07
申请号：US995295
申请日：1992-12-21
申请人： Peter Matyus , Klara Czako , Ildiko Varga , Andrea Jednakovics , Agnes Papp , Ilona Bodi , Gyorgy Rabloczky , Andras Varro , Laszlo Jaszlits , Aniko Miklos , Luca Levay , Gvorgy Schmidt , Marton Fekete , Maria Kurthy , Katalin Szemeredi , Erzsebet Zara
发明人： Peter Matyus , Klara Czako , Ildiko Varga , Andrea Jednakovics , Agnes Papp , Ilona Bodi , Gyorgy Rabloczky , Andras Varro , Laszlo Jaszlits , Aniko Miklos , Luca Levay , Gvorgy Schmidt , Marton Fekete , Maria Kurthy , Katalin Szemeredi , Erzsebet Zara
IPC分类号： A61K31/50 , A61K31/501 , A61K31/535 , A61K31/5377 , A61P9/06 , C07D237/14 , C07D237/22 , C07D403/04 , C07D403/06 , C07D413/06 , C07D413/14 , C07D237/10
CPC分类号： C07D237/14
摘要： Racemic or optically active new 3(2H)-pyridazinone derivatives, a process for the preparation thereof, pharmaceutical compositions comprising the same, to the use of the said 3(2H)-pyridazinone derivatives for the treatment of diseases and for the preparation of pharmaceutical compositions suitable for the treatment of diseases.The new 3(2H)-pyridazinone derivatives according to the invention correspond to the general formula (I), ##STR1##
摘要翻译：外消旋或光学活性的新的3（2H） - 哒嗪酮衍生物，其制备方法，包含它们的药物组合物，使用所述3（2H） - 哒嗪酮衍生物用于治疗疾病和用于制备药物适用于治疗疾病的组合物。根据本发明的新的3（2H） - 哒嗪酮衍生物对应于通式（I），（I）

9. 发明授权

US5240918A 2-(substituted imino)-thiazolidines and process for the preparation thereof 失效
标题翻译： 2-（取代的亚氨基） - 噻唑啉及其制备方法
公开(公告)号：US5240918A
公开(公告)日：1993-08-31
申请号：US857067
申请日：1992-03-24
申请人： Karoly Lempert , Gyula Hornyak , Jozsef Fetter , Antal Feller , Klara Gaso , Gabor Gigler , Laszlo Kapolnai , Lujza Petocz , Katalin Szemeredi , Marton Fekete
发明人： Karoly Lempert , Gyula Hornyak , Jozsef Fetter , Antal Feller , Klara Gaso , Gabor Gigler , Laszlo Kapolnai , Lujza Petocz , Katalin Szemeredi , Marton Fekete
IPC分类号： C07D277/18
CPC分类号： C07D277/18
摘要： The invention relates to new 2-(substituted imino)-thiazolidines, a process for the preparation thereof, pharmaceutical compositions comprising the same, the use of the said 2-(substituted imino)thiazolidines for the treatment of diseases and for the preparation of pharmaceutical compositions suitable for the treatment of diseases.The new 2-(substituted imino)-thiazolidine derivatives provided by the present invention correspond to the general formula (I), ##STR1## wherein R.sup.1 and R.sup.2 each represent halogen, nitro, C.sub.1-4 alkoxy or C.sub.1-4 alkyl, which latter may optionally carry one or more halogen substituent(s),R.sup.3 and R.sup.4 each represent hydrogen or C.sub.1-4 alkyl,Z denotes oxygen, sulfur or imino, which latter is substituted by a C.sub.1-6 alkyl or a C.sub.1-6 alkenyl group,R.sup.5 stands for hydrogen, C.sub.1-4 alkyl, C.sub.1-4 alkylthio or a group or the formula --NH--R, wherein R represents C.sub.1-6 alkyl, aryl, aralkyl or C.sub.1-6 alkenyl optionally carrying a halogen or a di-(C.sub.1-4 alkyl)-amino substituent; orZ and R.sup.5 together stand for a trivalent nitrogen atom, with the proviso that if Z denotes a substituted imino group, R.sup.5 stands for C.sub.1-4 alkylthio, and if R.sup.5 is C.sub.1-4 alkylthio, Z represents a substituted imino, and with the further proviso that if Z denotes sulfur, R.sup.5 is other than hydrogen or C.sub.1-4 alkyl,and possess valuable antianginal and analgesic properties.
摘要翻译：本发明涉及新的2-（取代的亚氨基） - 噻唑烷，其制备方法，包含该方法的药物组合物，所述2-（取代的亚氨基）噻唑烷用于治疗疾病和用于制备药物适用于治疗疾病的组合物。本发明提供的新的2-（取代亚氨基） - 噻唑烷衍生物对应于通式（I），其中R 1和R 2各自表示卤素，硝基，C 1-4烷氧基或C 1-4烷基，其可以任选地带有一个或多个卤素取代基，R 3和R 4各自表示氢或C 1-4烷基，Z表示氧，硫或亚氨基，后者被C 1-6烷基或C 1-6 烯基，R5代表氢，C1-4烷基，C1-4烷硫基或基团-NH-R，其中R表示C1-6烷基，芳基，芳烷基或任选携带卤素或二（C 1-4烷基） - 氨基取代基; 或Z和R5一起代表三价氮原子，条件是如果Z表示取代的亚氨基，则R5表示C1-4烷硫基，如果R5是C1-4烷硫基，则Z表示取代的亚氨基，并且与进一步的条件是，如果Z表示硫，R5不是氢或C1-4烷基，并且具有有价值的抗心绞痛和止痛特性。

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